CN115989229A - 5-氮杂-4’-硫代-2’-脱氧胞苷的多晶型物 - Google Patents

5-氮杂-4’-硫代-2’-脱氧胞苷的多晶型物 Download PDF

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Publication number
CN115989229A
CN115989229A CN202180052138.4A CN202180052138A CN115989229A CN 115989229 A CN115989229 A CN 115989229A CN 202180052138 A CN202180052138 A CN 202180052138A CN 115989229 A CN115989229 A CN 115989229A
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CN
China
Prior art keywords
crystalline polymorph
cancer
aza
days
effective amount
Prior art date
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Pending
Application number
CN202180052138.4A
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English (en)
Chinese (zh)
Inventor
M·J·苏托
郑斗瑛
李振洙
赵显龙
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pinot Bio Co ltd
Southern Research Institute
Original Assignee
Pinot Bio Co ltd
Southern Research Institute
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Publication of CN115989229A publication Critical patent/CN115989229A/zh
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/12—Triazine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN202180052138.4A 2020-07-23 2021-07-23 5-氮杂-4’-硫代-2’-脱氧胞苷的多晶型物 Pending CN115989229A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063055754P 2020-07-23 2020-07-23
US63/055,754 2020-07-23
PCT/US2021/043021 WO2022020747A1 (en) 2020-07-23 2021-07-23 Polymorophs of 5-aza-4'-thio-2-deoxycytidine

Publications (1)

Publication Number Publication Date
CN115989229A true CN115989229A (zh) 2023-04-18

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ID=79687860

Family Applications (1)

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CN202180052138.4A Pending CN115989229A (zh) 2020-07-23 2021-07-23 5-氮杂-4’-硫代-2’-脱氧胞苷的多晶型物

Country Status (10)

Country Link
US (1) US11447472B2 (https=)
EP (1) EP4185583A4 (https=)
JP (1) JP7679452B2 (https=)
KR (1) KR102866823B1 (https=)
CN (1) CN115989229A (https=)
AU (1) AU2021314329A1 (https=)
BR (1) BR112023001236A2 (https=)
CA (1) CA3186696A1 (https=)
MX (1) MX2023000979A (https=)
WO (1) WO2022020747A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20230123277A1 (en) * 2021-10-15 2023-04-20 Akirabio, Inc. Compositions comprising 2'-deoxycytidine analogs and use thereof for the treatment of sickle cell disease and thalassemia

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101014246A (zh) * 2004-07-13 2007-08-08 苏伯俭股份有限公司 地西他滨多晶型物的组合物和制剂及其使用方法
WO2019152459A1 (en) * 2018-02-01 2019-08-08 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Stereoselective synthesis and process for the manufacturing of 2'-deoxynucleosides
WO2019204637A1 (en) * 2018-04-19 2019-10-24 Southern Research Institute 4'-thio-nucleotide and -nucleoside prodrugs for the treatment of cancer

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6020322A (en) 1993-11-09 2000-02-01 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
US5591722A (en) 1989-09-15 1997-01-07 Southern Research Institute 2'-deoxy-4'-thioribonucleosides and their antiviral activity
CN103951583B (zh) * 2006-12-06 2016-01-06 科内图斯医药公司 一种抑制剂的结晶形式
PL3692983T3 (pl) 2008-05-15 2021-12-27 Celgene Corporation Doustne formulacje analogów cytydyny i sposoby ich zastosowania
WO2011109012A1 (en) 2010-03-02 2011-09-09 Southern Research Institute Use of 2'-deoxy-4'-thiocytidine and its analogues as dna hypomethylating anticancer agents
US20110218170A1 (en) 2010-03-02 2011-09-08 Southern Research Institute Use of 2'-deoxy-4'-thiocytidine and its analogues as dna hypomethylating anticancer agents
SG11201610551TA (en) 2014-07-14 2017-01-27 Gilead Sciences Inc Combinations for treating cancers
US20160312261A1 (en) 2015-04-24 2016-10-27 Plasmia Biotech, S.L. Enzymatic production of cytosinic nucleoside analogues
EP3527226A4 (en) 2016-10-17 2020-06-17 Daiichi Sankyo Company, Limited COMBINATION THERAPY PROCEDURE WITH MDM2 INHIBITOR AND DNA METHYL TRANSFERASE INHIBITOR

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101014246A (zh) * 2004-07-13 2007-08-08 苏伯俭股份有限公司 地西他滨多晶型物的组合物和制剂及其使用方法
WO2019152459A1 (en) * 2018-02-01 2019-08-08 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Stereoselective synthesis and process for the manufacturing of 2'-deoxynucleosides
WO2019204637A1 (en) * 2018-04-19 2019-10-24 Southern Research Institute 4'-thio-nucleotide and -nucleoside prodrugs for the treatment of cancer

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
THOTTASSERY, JV ET AL.: "Novel DNA methyltransferase‑1 (DNMT1) depleting anticancer nucleosides, 4′-thio-2′-deoxycytidine and 5-aza-4′-thio-2′-deoxycytidine", CANCER CHEMOTHERAPY AND PHARMACOLOGY, vol. 74, no. 2, 8 June 2014 (2014-06-08), pages 291 - 302, XP093163393, DOI: 10.1007/s00280-014-2503-z *
TIWARI, KN ET AL.: "Synthesis and Anti-cancer Activity of Some Novel 5-Azacytosine Nucleosides", NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS, vol. 22, no. 12, 31 December 2003 (2003-12-31), pages 2161 - 2170, XP055221323, DOI: 10.1081/NCN-120026872 *

Also Published As

Publication number Publication date
MX2023000979A (es) 2023-04-20
JP7679452B2 (ja) 2025-05-19
EP4185583A4 (en) 2024-10-30
CA3186696A1 (en) 2022-01-27
KR102866823B1 (ko) 2025-09-30
EP4185583A1 (en) 2023-05-31
WO2022020747A1 (en) 2022-01-27
US11447472B2 (en) 2022-09-20
AU2021314329A1 (en) 2023-02-23
AU2021314329A8 (en) 2023-03-09
JP2023535724A (ja) 2023-08-21
KR20230061354A (ko) 2023-05-08
WO2022020747A8 (en) 2023-02-16
BR112023001236A2 (pt) 2023-04-04
US20220024903A1 (en) 2022-01-27

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Application publication date: 20230418